Lomitapide mesylate is a microsomal triglyceride transfer protein inhibitor marketed as JUXTAPID® or LOJUXTA® in US and Europe respectively. It is represented by the following formula

It is indicated as an adjunct to low fat diet to reduce low density lipoprotein cholesterol, total cholesterol, apolipoprotein B and nonhigh density lipoprotein cholesterol in patients with homozygous familial hypercholesterolemia.
The discovery of new amorphous forms of active pharmaceutical ingredients (“APIs”) provides opportunities to improve the performance characteristics, the solubility, stability, flowability, tractability and compressibility of drug substances. Amorphous form of a drug provides solubility advantage as compared to the crystalline forms and hence offers opportunities for solubility and bioavailability enhancement.
The present invention provides novel amorphous form of lomitapide mesylate and process of preparation thereof.
Advantageously the amorphous lomitapide mesylate of the present invention does not contain genotoxic alkyl mesylate impurities like methyl mesylate and isopropyl mesylate.